|Systematic (IUPAC) name|
|AHFS/Drugs.com||Consumer Drug Information|
|Injection and oral|
|Biological half-life||3.1 h|
|ATC code||B02AA02 (WHO)|
|Molar mass||157.21 g/mol|
Tranexamic acid (TXA) is a medication used to treat or prevent excessive blood loss from trauma, surgery, and in various medical conditions including hemophilia and heavy menstrual bleeding. It comes in oral and intravenous forms.
Side effects are uncommon and include gastrointestinal effects, dizziness, fatigue, headache, and hypersensitivity reactions. The medication needs to be used cautiously in people with kidney disease and who are at a high risk for blood clots. Tranexamic is safe to use in pregnant women. However, caution should be used in lactating women. It is an antifibrinolytic.
It was discovered in 1962 by Utako Okamoto and has been on the World Health Organization's List of Essential Medicines, the most important medications needed in a basic health system.
Tranexamic acid is frequently used following major trauma. Tranexamic acid is used to prevent and treat blood loss in a variety of situations, such as dental procedures for hemophiliacs, heavy menstrual bleeding, and surgeries with high risk of blood loss.
Heavy menstrual bleeding
Tranexamic acid is used to treat heavy menstrual bleeding. When taken by mouth it both safely and effectively treats regularly occurring heavy menstrual bleeding. Another study demonstrated that the dose does not need to be adjusted in females who are between ages 12 and 16.
- Tranexamic acid is used in orthopedic surgery to reduce blood loss, to the extent of reducing or altogether abolishing the need for perioperative blood collection. It is of proven value in clearing the field of surgery and reducing blood loss when given before or after surgery. Drain and number of transfusions are reduced.
- In surgical corrections of craniosynostosis in children it reduces the need for blood transfusions.
- In spine surgery, e.g. scoliosis correction with posterior spinal fusion using instrumentation, to prevent excessive blood loss.
- In cardiac surgery, both with and without cardiopulmonary bypass e.g. coronary artery bypass surgery, it is used to prevent excessive blood loss. It replaces aprotinin.
In the United States, tranexamic acid is FDA approved for short-term use in people with severe bleeding disorders who are about to have dental surgery. Tranexamic acid is used for a short period of time before and after the surgery to prevent major blood loss and decrease the need for blood transfusions. In people with hemophilia, combinations of tranexamic acid and factor VII or IX have effectively decreased blood loss and the need for transfusions after dental surgery In one person with mild hemophilia, a combination of tranexamic acid and demopressin effectively stopped bleeding
Tranexamic acid is used in dentistry in the form of a 5% mouth rinse after extractions or surgery in patients with prolonged bleeding time, e.g. from acquired or inherited disorders.
- In obstetrics, tranexamic acid is used after delivery to reduce bleeding, often with syntocinon/oxytocin and fundal massage. Since 2010, the WOMAN (World Maternal Antifibrinolytic) trial has been in progress worldwide to establish the efficacy of the drug to arrest postpartum haemorrhage (PPH) in 15 000 women, due to be completed in 2016. Since the drug can be administered orally, it has great potential to reduce maternal mortality rates in developing countries where primary healthcare is often unavailable.
- In hereditary angioedema
- In hereditary hemorrhagic telangiectasia - Tranexamic acid has been shown to reduce frequency of epistaxis in patients suffering severe and frequent nosebleed episodes from hereditary hemorrhagic telangiectasia.
- In melasma - Tranexamic acid has shown to provide rapid and sustained lightening in melasma by decreasing melanogenesis in epidermal melanocytes.
- In hyphema - Tranexamic acid has been shown to be effective in reducing risk of secondary hemorrhage outcomes in patients with traumatic hyphema.[needs update]
Common side effects include:
- Headaches (50.4 - 60.4%)
- Back aches (20.7 - 31.4%)
- Nasal sinus problem (25.4%)
- Abdominal pain (12 - 19.8%)
- Diarrhea (12.2%)
- Fatigue (5.2%)
- Anemia (5.6%)
Rare side effects include:
- Tranexamic acid is categorized as pregnancy category B. No harm has been found in animal studies.
- Small amounts appears in breast milk if taken during lactation. If it is required for other reasons, breastfeeding may be continued.
- Tranexamic acid is also not indicated for postmenopausal women and geriatrics.
- In kidney impairment, tranexamic acid is not well studied. However, due to the fact that it is 95% excreted unchanged in the urine, it should be dose adjusted in patients with renal impairment.
- In liver impairment, dose change is not needed as only a small amount of the drug is metabolized through the liver.
Mechanism of action
Tranexamic acid is a synthetic analog of the amino acid lysine. It serves as an antifibrinolytic by reversibly binding four to five lysine receptor sites on plasminogen or plasmin. This prevents plasmin from binding to and degrading fibrin and preserves the framework of fibrin's matrix structure. Tranexamic acid has roughly eight times the antifibrinolytic activity of an older analogue, ε-aminocaproic acid.
Society and culture
TXA was discovered in 1962 by Utako Okamoto. It has been included in the WHO list of essential medicines. TXA is inexpensive and treatment would be considered highly cost effective in high, middle and low income countries.
Tranexamic acid is marketed in the U.S. and Australia in tablet form as Lysteda and in IV form as Cyklokapron and Transamin, in the UK as Cyclo-F and Femstrual, in Asia as Transcam, in Bangladesh as Traxyl, in India as Pause, in South America as Espercil, in Japan as Nicolda, in France and Romania as Exacyl and in Egypt as Kapron. In the Philippines, its capsule form is marketed as Hemostan and In Israel as Hexakapron.
The U.S. Food and Drug Administration (FDA) approved tranexamic acid oral tablets (brand name Lysteda) for treatment of heavy menstrual bleeding on 13 November 2009.
In March 2011 the status of tranexamic acid for treatment of heavy menstrual bleeding was changed in the UK, from PoM (Prescription only Medicines) to P (Pharmacy Medicines) and became available over the counter in UK pharmacies under the brand names of Cyklo-F and Femstrual, initially exclusively for Boots pharmacy, which has sparked some discussion about availability. (In parts of Europe - like Sweden - it had then been available OTC for over a decade.) Regular liver function tests are recommended when using tranexamic acid over a long period of time.
- "Cyklokapron (tranexamic acid) Product Information" (PDF). Retrieved 3 November 2015.
- "Lysteda (tranexamic acid) Package Insert" (PDF). accessdata.FDA.gov. Retrieved 2 November 2015.
- Geoff Watts (2016). "Obituary Utako Okamoto". The Lancet 387 (10035): 2286. doi:10.1016/S0140-6736(16)30697-3.
- "19th WHO Model List of Essential Medicines (April 2015)" (PDF). WHO. April 2015. Retrieved May 10, 2015.
- Binz, S; McCollester, J; Thomas, S; Miller, J; Pohlman, T; Waxman, D; Shariff, F; Tracy, R; Walsh, M (2015). "CRASH-2 Study of Tranexamic Acid to Treat Bleeding in Trauma Patients: A Controversy Fueled by Science and Social Media.". Journal of blood transfusion 2015: 874920. doi:10.1155/2015/874920. PMID 26448897.
- Melvin, JS; Stryker, LS; Sierra, RJ (22 October 2015). "Tranexamic Acid in Hip and Knee Arthroplasty.". The Journal of the American Academy of Orthopaedic Surgeons 23: 732–40. doi:10.5435/JAAOS-D-14-00223. PMID 26493971.
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- RCPCH. "Evidence Statement Major trauma and the use of tranexamic acid in children Nov 2012" (PDF). Retrieved 17 December 2012.
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- Karn, D; Kc, S; Amatya, A; Razouria, E. A.; Timalsina, M (2012). "Oral tranexamic acid for the treatment of melasma". Kathmandu University Medical Journal 10 (40): 40–3. doi:10.3126/kumj.v10i4.10993. PMID 23575051.
- Gharaibeh, Almutez; Savage, Howard I; Scherer, Roberta W; Goldberg, Morton F; Lindsley, Kristina (2011). "Medical interventions for traumatic hyphema". Cochrane Database of Systematic Reviews (1): CD005431. doi:10.1002/14651858.CD005431.pub2. PMC 3437611. PMID 21249670.
- "Tranexamic Acid use while Breastfeeding". www.drugs.com. 7 Nov 2014. Retrieved 27 May 2016.
- Guerriero, Carla; Cairns, John; Perel, Pablo; Shakur, Haleema; Roberts, Ian; Crash 2 Trial, Collaborators (2011). "Cost-Effectiveness Analysis of Administering Tranexamic Acid to Bleeding Trauma Patients Using Evidence from the CRASH-2 Trial". PLoS ONE 6 (5): e18987. Bibcode:2011PLoSO...618987G. doi:10.1371/journal.pone.0018987. PMC 3086904. PMID 21559279.
- Tranexamic Acid to be available OtC[full citation needed]
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